428468-34-2Relevant academic research and scientific papers
Accurate sequence stimuli-responsive polymer as well as preparation method and application thereof
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, (2021/04/17)
The invention provides an accurate sequence stimuli-responsive polymer as well as a preparation method and application thereof. The polymer has a structure shown in a formula I in the specification. The polymer induces a trigger element to break under corresponding stimulation conditions, and then spontaneous sequential depolymerization is carried out through electron rearrangement. Compared with most stimulus-responsive polymers researched at present, the polymer has the advantages that the number of repeated units is determined, the sequence is controllable, and the preparation method is efficient in reaction, short in reaction time and high in yield. According to the characteristics of the accurate polymer, the polymer is expected to be used in the application fields of signal amplification, degradable nano materials, sensing application devices, drug delivery, controllable release and the like.
Design, synthesis and antiproliferative activities evaluation of thiazolopyrimidines derivatives through biginelli reaction
Zhu, Pengju,Fu, Huansheng,Fang, Hao
, p. 1382 - 1390 (2017/12/28)
Background: Thiazolopyrimidines possessed their structural diversity and various biological activity. Up to date, thiazolopyrimidines derivatives have widespread applications in pharmaceutical fields. In this article, a series of thiazolopyrimidine derivatives were designed based on the lead compound structure in our previous studies. Methods: All the target compounds were synthesized with the coupling reaction, Biginelli reaction and “one-pot” aldol condensation. Their structures were identified by1H NMR,13C NMR spectra and HRMS. Antitumor activities of the target compounds were evaluated by MTT. Results: 25 new target compounds were synthesized and they primarily screened through testing their inhibitory rates against two human tumor cell lines and Compounds 15, 17, 20, 22, 40 exhibited more than 70% inhibitory rate against both MDA-MB-231 and K562. Further assessing their IC50 against five tumor cell lines, 15 and 22 show advantage over lead compound I in MDA-MB-231, K562 and PC-3. Conclusion: A series of thiazolopyrimidine derivatives were synthesized and the preliminary biological evaluation suggest that target compound 22 exhibited better antiproliferative activity against K562 than gossypol.
Identification of para-Substituted Benzoic Acid Derivatives as Potent Inhibitors of the Protein Phosphatase Slingshot
Li, Kang-Shuai,Xiao, Peng,Zhang, Dao-Lai,Hou, Xu-Ben,Ge, Lin,Yang, Du-Xiao,Liu, Hong-Da,He, Dong-Fang,Chen, Xu,Han, Ke-Rui,Song, Xiao-Yuan,Yu, Xiao,Fang, Hao,Sun, Jin-Peng
, p. 1980 - 1987 (2015/12/23)
Slingshot proteins form a small group of dual-specific phosphatases that modulate cytoskeleton dynamics through dephosphorylation of cofilin and Lim kinases (LIMK). Small chemical compounds with Slingshot-inhibiting activities have therapeutic potential against cancers or infectious diseases. However, only a few Slingshot inhibitors have been investigated and reported, and their cellular activities have not been examined. In this study, we identified two rhodanine-scaffold-based para-substituted benzoic acid derivatives as competitive Slingshot inhibitors. The top compound, (Z)-4-((4-((4-oxo-2-thioxo-3-(o-tolyl)thiazolidin-5-ylidene)methyl)phenoxy)methyl)benzoic acid (D3) had an inhibition constant (Ki) of around 4 μm and displayed selectivity over a panel of other phosphatases. Moreover, compound D3 inhibited cell migration and cofilin dephosphorylation after nerve growth factor (NGF) or angiotensin II stimulation. Therefore, our newly identified Slingshot inhibitors provide a starting point for developing Slingshot-targeted therapies.
